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Toceranib Phosphate

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Catalog No. T7394Cas No. 874819-74-6
Alias SU11654 phosphate, PHA 291639 phosphate

Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR

Toceranib Phosphate

Toceranib Phosphate

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Purity: 98.56%
Catalog No. T7394Alias SU11654 phosphate, PHA 291639 phosphateCas No. 874819-74-6
Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$41-In Stock
25 mg$68-In Stock
50 mg$85-In Stock
100 mg$110-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:98.56%
Appearance:Solid
Color:Orange
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Product Introduction

Bioactivity
Description
Toceranib Phosphate (SU11654 phosphate), is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR
Targets&IC50
FLK1:6 nM (Ki), PDGFRβ:5 nM (Ki)
In vivo
Systolic blood pressure was significantly (P = 0.0013) higher in previously normotensive treatment dogs after initiation of treatment with toceranib phosphate (152 mmHg ± 19) compared to baseline (136 mmHg ± 14). 37% of treated dogs developed SBP ≥ 160 mmHg. The prevalence of systemic hypertension (37%) and proteinuria (21%) at baseline in treatment dogs did not differ from that of age-matched healthy controls (15% [P = 0.13] and 0% [P = 0.069], respectively)[1].
Animal Research
Dogs scheduled to received toceranib phosphate treatment were divided into 2 groups based on SBP recorded at screening: dogs that were normotensive were assigned to Group 2a and dogs diagnosed with HT were assigned to Group 2b. After baseline evaluation, dogs enrolled in Group 2a received toceranib phosphate at a standard dose as previously published.2 Group 2b dogs received toceranib phosphate as described, but were also treated with standard‐of‐care treatment for HT, including amlodipine besylate (0.2–0.4 mg/kg PO q 24 hours), enalapril maleate (0.5 mg/kg PO q 12 hours), or both, initiated at the discretion of the attending veterinarian. Some dogs were treated with additional medications, including corticosteroids, at the discretion of the oncologist. All dogs were re‐evaluated on Day 14 (±3 days) at which time a UPC and blood pressure measurements were performed[1].
SynonymsSU11654 phosphate, PHA 291639 phosphate
Chemical Properties
Molecular Weight494.45
FormulaC22H28FN4O6P
Cas No.874819-74-6
SmilesOP(O)(O)=O.Cc1[nH]c(\C=C2/C(=O)Nc3ccc(F)cc23)c(C)c1C(=O)NCCN1CCCC1
Relative Density.no data available
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: Slightly soluble

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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